Title
First demonstration of in vivo mapping for regional brain monoacylglycerol lipase using PET with [11C]SAR127303.
Abstract
Abstract Monoacylglycerol lipase (MAGL) is a main regulator of the endocannabinoid system within the central nervous system (CNS). Recently, [ 11 C]SAR127303 was developed as a promising radioligand for MAGL imaging. In this study, we aimed to quantify regional MAGL concentrations in the rat brain using positron emission tomography (PET) with [ 11 C]SAR127303. An irreversible two-tissue compartment model (2-TCMi, k 4  = 0) analysis was conducted to estimate quantitative parameters ( k 3 , K i 2-TCMi , and λk 3 ). These parameters were successfully obtained with high identifiability (  striatum u003e hippocampus u003e thalamus u003e cerebellum u003e hypothalamus ≈ pons. In vitro autoradiographs using [ 11 C]SAR127303 showed a heterogeneous distribution of radioactivity, as seen in the PET images. The K i 2-TCMi and λk 3 values correlated relatively highly with in vitro binding ( r  u003e 0.4, P K i 2-TCMi values showed high correlation and low underestimation ( K i Patlak ). In conclusion, we successfully estimated regional net uptake value of [ 11 C]SAR127303 reflecting MAGL concentrations in rat brain regions for the first time.
Year
Venue
Field
2018
NeuroImage
Central nervous system,Regulator,Neuroscience,Radioligand,In vitro,Psychology,Cognitive psychology,In vivo,Positron emission tomography,Endocannabinoid system,Monoacylglycerol lipase
DocType
Volume
Citations 
Journal
176
0
PageRank 
References 
Authors
0.34
0
12